摘要
目的优化O-去甲基文拉法辛的合成工艺。方法以对羟基苯乙酸为原料,经苄基保护,依次经过酰化、缩合、还原、氢解脱苄、成盐反应成功合成了目标化合物。结果反应条件得到了优化,避免了使用二甲胺气体、正丁基锂和四氢锂铝试剂,总收率为30%(以对羟基苯乙酸计)。结论该路线原料价廉易得,反应条件温和,操作简便,适合于工业化生产。目标化合物经1 H-NMR、MS结构确证。
Objective To optimize the synthesis of O-desmethylvenlafaxine.Methods The 2-（4-hydroxyphenyl） acetic acid was used as starting material,which was etherified by benzyl bromide via etherification reaction.O-desmethylvenlafaxine succinate was synthesized by amidation,condensation,reduction,hydrolysis,and salt formation reaction.Results The synthetic process avoided using dimethylamine,n-butyllithium,and lithium aluminum hydride.The total yield was 30%.Conclusion The synthetic route is simple and economic.The reaction condition is mild and suitable for industrial production.The structure of O-desmethylvenlafaxine succinate is elucidated by 1H-NMR and MS.
出处
《中南药学》
CAS
2012年第3期175-177,共3页
Central South Pharmacy
